IMD-0354

IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity^[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC₅₀ of 1.2 uM^[2]. IC50 & Target: IKKβ^[1]
IC50: 1.2±0.3 μM (NF-κB)^[2] In Vitro: IMD-0354 inhibits NF-κB activity in HMC-1 cells, resulting in complete repression of growth factor-independent proliferation of mast cells. When the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354, cell proliferation is completely suppressed. HMC-1 cells are incubated with increasing concentrations of IMD-0354 or STI571 for 24, 48, and 72 hours, and numbers and viability of cells are determined by a dye exclusion test and an MTT assay. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner. The inhibitory effect of IMD-0354 is remarkable, even at lower concentrations, when compared with that of STI571^[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC ₅₀ of 1.2±0.3 uM^[2]. In Vivo: Daily administration with 5 mg/kg IMD-0354 significantly suppresses tumor expansion in nude mice implanted with established MDA-MB-231 tumors. In mice treated with IMD-0354, tumor progression is restrained^[3]. The number of infiltrating cells in aqueous humor is 53.6±9.8×10⁵, 72.5±17.0×10⁵, 127.25±32.0×10⁵, and 132.0±25.0×10⁵ cells/mL in rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, respectively. The total protein concentrations of aqueous humor are 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.33±1.8 mg/mL in rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively^[4].